Overview
11 DESCRIPTION SAJAZIR (icatibant) is a synthetic decapeptide with five non-proteinogenic amino acids. The chemical structure of icatibant acetate is presented in Figure 1. Figure 1 Chemical Structure Chemical name: D-Arginyl-L-arginyl-L-prolyl-L[(4R)-4-hydroxyprolyl]-glycyl-L[3-(2-thienyl)alanyl]-L-seryl-D-(1,2,3,4-tetrahydroisoquinolin-3-ylcarbonyl)-L[(3aS,7aS)-octahydroindol-2-ylcarbonyl]-L-arg...
Mechanism of Action
12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action Icatibant is a competitive antagonist selective for the bradykinin B2 receptor, with an affinity similar to bradykinin. Hereditary angioedema is caused by an absence or dysfunction of C1-esterase-inhibitor, a key regulator of the Factor XII/kallikrein proteolytic cascade that leads to bradykinin production. Bradykinin is a vasodilator which is thought to be responsible for the characteristic HAE symptoms of localized swelling, inflammation, and pain. Icatibant inhibits bradykinin from binding the B2 receptor and thereby treats the clinical symptoms of an acute, episodic attack of HAE. 12.
Indications
- 1 INDICATIONS AND USAGE SAJAZIR (icatibant) injection is indicated for the treatment of acute attacks of hereditary angioedema (HAE) in adults 18 years of age and older. SAJAZIR (icatibant) injection is a bradykinin B2 receptor antagonist indicated for treatment of acute attacks of hereditary angioedema (HAE) in adults 18 years of age and older. ( 1 )
Common Doses
- 30 mg
Dosage
2 DOSAGE AND ADMINISTRATION 30 mg injected subcutaneously in the abdominal area. ( 2.1 ) If response is inadequate or symptoms recur, additional injections of 30 mg may be administered at intervals of at least 6 hours. ( 2.1 ) Do not administer more than 3 injections in 24 hours. ( 2.1 ) Patients may self-administer upon recognition of an HAE attack. ( 2.2 ) 2.1 Recommended Dosing The recommended dose of SAJAZIR is 30 mg administered by subcutaneous (SC) injection in the abdominal area.
Contraindications
- 4 CONTRAINDICATIONS None. None. ( 4 )
Side Effects
- 6 ADVERSE REACTIONS The most commonly reported adverse reactions were injection site reactions, which occurred in almost all patients (97%) in clinical trials. Other common adverse reactions occurring in greater than 1% of patients included pyrexia, transaminase increase, dizziness, and rash. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Cycle Pharmaceuticals Ltd at 1-800-836-4380 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch 6.
Interactions
- 7 DRUG INTERACTIONS 7.1 ACE Inhibitors Icatibant is a bradykinin B2 receptor antagonist and thereby has the potential to have a pharmacodynamic interaction with ACE inhibitors where icatibant may attenuate the antihypertensive effect of ACE inhibitors. Clinical trials to date have excluded subjects taking ACE inhibitors.